Sunitinib Malate

Licensed by Pfizer Catalog No.S1042

Sunitinib Malate Chemical Structure

Molecular Weight(MW): 532.56

Sunitinib Malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit.

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In DMSO USD 191 In stock
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USD 147 In stock
USD 447 In stock
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Cited by 42 Publications

12 Customer Reviews

  • PDGF-AA induces Ezh2 expression and proliferation in juvenile islets but not in adult islets. Western immunoblots of indicated islet proteins from 3 week or 9 month-old WT islets 2 days after exposure to PDGF-AA alone, or PDGF-AA plus RTK inhibitors Sunitinib.

    Nature 2011 478(7369):349-55. Sunitinib Malate purchased from Selleck.

    Assessment of effects on human juvenile or adult islets after exposure to PDGF-AA (50 ng/ml) for 2 days, with or without Sunitinib (2 uM) or U0126 (10 uM)co-treatment. Average percentage of BrdU+ insulin+ cells was morphometry from sectioned islets immunostained for insulin (green), glucagon (white) and BrdU (red). n = 3-6 independent experiments.

    Nature 2011 478(7369):349-55. Sunitinib Malate purchased from Selleck.

  • Combinational treatment of kinase inhibitors induces the similar phenotype produced by PP1. All images are lateral view with dorsal to the top and anterior to the left. The combinational treatment of Dasatinib (D) or U0126 (U) with Sunitinib (SU),PTK787 (PTK), or ZM323881 (Z) resulted in the shrinkage of dorsal aorta.

    Cell Res 2011 21, 1080-1087. Sunitinib Malate purchased from Selleck.

    A, Tumor growth curves from the initial sunitinib drug trials, with endpoint set at 1,300 mm3 (mean ± SEM). Measurements began one week after tumor inoculation and on the day sunitinib treatment began. Subsequent experimental endpoints were set on the basis of these growth curves and their intersections with this data are shown. B, Histogram plot showing the distribution of tumor sizes at day 8 of treatment. Sunitinib-treated tumors exceeding 250 mm3 in size were identified as falling into the nonresponsive cohort. Sunitinib treatment significantly retards growth of responsive tumors.

    Cancer Res, 2017, 77(4):1008-1020 . Sunitinib Malate purchased from Selleck.

  • Sunitinib decreases FLT-3 and RET phosphor ylation but increases ERK phosphorylation in a time-dependent manner. H295R and SW13 cells were treated with sunitinib (10 nM) for various time points as indi-cated. Cell lysates were prepared and phospho-FLT-3, RET, and ERK levels were monitored by Western Blot-ting. Re-probing against FLT-3, RET, and ERK was done to ensure equal protein loading.

    Surgery 2012 152, 1045-50. Sunitinib Malate purchased from Selleck.

    Sunitinib or PD98059 decreases cell proliferation in a dose-dependent manner. H295R and SW13 cells were treated with various concentration of sunitinib or PD98059 for 48 hours as indicated. Treated cells were subjected to the MTS proliferation assay. Similar experiments were repeated 3 times. Histograms represent relative % of OD490 nm absorbance (* P < .05). All data are relative multiples of expression compared with untreated cells. The data are representative of three experiments and are expressed as the mean ?SE.

    Surgery 2012 152, 1045-50. Sunitinib Malate purchased from Selleck.

  • Autophagic activation in sunitinib- and sorafenib- but not AZD6244-treated cells. Medullary thyroid cancer-1.1 (MTC-1.1; A) and TT ( B) cells were treated with dimethyl sulfoxide (DMSO), sunitinib (50 nM), sorafenib (10 nM), AZD6244 (30 nM), or everolimus (20 nM) for 48 hours. Cell lysates were prepared, and light chain 3 (LC3)-I and -II cleaved caspase-3 protein levels were monitored by Western blotting. Reprobing against actin was per formed to ensure equal protein loading. ( C ) MTC-1.1 and TT cells were transiently transfected with autophagy protein 5 (Atg-5) small inter fering RNA. Transfection with scrambled small inter fering RNA was used as a control. After transfection, cells with and without Atg-5 knockdown were exposed to DMSO or 20 nM of everolimus for 48 hours. Cell lysates were pre- pared and LC3-I and -II protein expression levels were monitored by Western blotting. Reprobing against Atg-5 was per formed to monitor Atg-5 knockdown efficiency. Reprobing against actin was per formed to ensure equal protein.

    Surgery 2012 152, 1142-9. Sunitinib Malate purchased from Selleck.

    Autophagy inhibition blocks the antiproliferative effects of sunitinib and sorafenib but not AZD6244. Medullary thyroid cancer–1.1 (MTC-1.1) and TT cells were transfected transiently with scrambled or autophagy protein 5 (Atg-5) small inter fering RNA. After transfection, cells with and without Atg-5 knockdown were exposed to sunitinib (50 nM), sorafenib (10 nM), and AZD6244 (30 nM) for 48 hours. Treated cells were subjected to a 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium proliferation assay. Similar experiments were repeated 3 times. Histograms represent the relative percent of OD490 nM absorbance. The asterisk indicates significance versus scrambled small inter fering RNA–treated control ( P < .05). All data are relative multiples of expression compared to untreated cells. The data are representative of 3 experiments and are expressed as the mean ± the standard error.

    Surgery 2012 152, 1142-9. Sunitinib Malate purchased from Selleck.

  • Sunitinib limits the colonial growth of HT-29 by downregulating HIF-1a. (A) The number and size of colonies formed in soft agar. The numbers of small colonies (<50 μm diameter) were not different among conditions of a serial concentration of sunitinib. On the contrary, large colonies (>50 μm diameter) disappeared after incubation with sunitinib. Each point represents the mean and SD from four separate experiments. (B) HIF-1a expression and hypoxia within HT-29 colony. After colonies grew for 4 weeks, HIF-1a and hypoxia were visualized by immunofluoroscence staining. Bar = 20 μm.

    Biochem Bioph Res Co 2010 398, 205–211. Sunitinib Malate purchased from Selleck.

    2. Sunitinib downregulates HIF-1a. (A) Dose-dependent repression of HIF-1a protein level by sunitinib in HT-29. HT-29 cells were incubated under normoxic (N) or hypoxic (H) conditions in the presence of sunitinib for 24 h. HIF-1a and ARNT proteins in total cell lysates were analyzed by Western blotting. (B) Sunitinib attenuates the hypoxic induction of HIF-1 target genes. RNAs were isolated from HT-29 cells subjected to normoxia (N) or hypoxia (H) in the presence of sunitinib for 16 h. The mRNAs of HIF-1a and its target genes were analyzed by RT-PCR and autoradiography. PGK1 indicates phosphoglycerate kinase 1; PDK1, pyruvate dyhydrogenase kinase 1; CAIX, carbonic anhydrase IX. (C) Sunitinib-induced HIF-1 inhibition. Epo-enhancer and b- galactosidase reporter plasmids were co-transfected into HEK293 cells. After 16 h incubation, luciferase and b-galactosidase activities were measured. *P < .05 versus the hypoxic control.

     

     

    Biochem Bioph Res Co 2010 398, 205–211. Sunitinib Malate purchased from Selleck.

  • Sunitinib inhibits 50-UTR-dependent translation of HIF-1a. (A) 50 cap-dependent translational activity of HIF-1a. The luciferase reporter plasmid contains the HIF-1a 50-UTR segment between the tk promoter and the luciferase gene. HT-29 cells were co-transfected with the reporter plasmid (8 lg per 100-mm dish) and the b-gal plasmid (4 μg). After 16 h incubation under normoxic or hypoxic conditions with sunitinib, cells were lysed and subjected to luciferase assay. *P < .05 versus the hypoxic control. (B) IRES-dependent translational activity of HIF-1a. The luciferase reporter plasmid contains the HIF-1a 50-UTR segment between the GFP gene and the luciferase gene. HT-29 cells were co-transfected with the reporter plasmid (8 μg) and the b-gal plasmid (4 μg). *P < .05 versus the hypoxic control. (C) Sunitinib inhibits phosphorylation of Akt. After 8 h incubation under hypoxic condition with sunitinib, HT-29 cells were lysed and subjected to Western blotting. (D) Sunitinib suppresses HIF-1a in VHL-null RCC4 cells. VHL (-/-) RCC4 cells were incubated under normoxic conditions sunitinib for 8 h, and HIF-1a in total cell lysates was analyzed by Western blotting.

     

     

    Biochem Bioph Res Co 2010 398, 205–211. Sunitinib Malate purchased from Selleck.

    Experimental layout for VEGF signaling blocking and LCMV infection in WT mice. Mice received two injections on day 0 and 3 p.i. of Abs as described in Material and Methods, or daily gavage of the VEGFR/PDGFR-inhibitor sunitinib. Inguinal LN volume on day 0 (D0) or day 8 (D8) p.i. after treatment of mice with control Ig or anti-VEGFR2, anti-VEGF-A Abs or sunitinib. Pooled from 1-2 independent experiments with 3-5 mice per treatment. D. Total HEV length on day 0 (D0) or day 8 (D8) p.i. as in C. No significant difference was found in C and D between day 8 control Ig and Ab- or inhibitor-treated values (One-way ANOVA).

    AACR Sunitinib Malate purchased from Selleck.

Purity & Quality Control

Choose Selective PDGFR Inhibitors

Biological Activity

Description Sunitinib Malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit.
Targets
Kit [1]
(Cell-free assay)
FLT3 [1]
(Cell-free assay)
PDGFRβ [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
2 nM 80 nM
In vitro

Sunitinib also potently inhibits Kit and FLT-3. [1] Sunitinib is a potent ATP-competitive inhibitor of VEGFR2 (Flk1) and PDGFRβ with Ki of 9 nM and 8 nM, respectively, displaying >10-fold higher selectivity for VEGFR2 and PDGFR than FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, and src. In serum-starved NIH-3T3 cells expressing VEGFR2 or PDGFRβ, Sunitinib inhibits VEGF-dependent VEGFR2 phosphorylation and PDGF-dependent PDGFRβ phosphorylation with IC50 of 10 nM and 10 nM, respectively. Sunitinib inhibits VEGF-induced proliferation of serum-starved HUVECs with IC50 of 40 nM, and inhibits PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRβ or PDGFRα with IC50 of 39 nM and 69 nM, respectively. [2] Sunitinib inhibits phosphorylation of wild-type FLT3, FLT3-ITD, and FLT3-Asp835 with IC50 of 250 nM, 50 nM, and 30 nM, respectively. Sunitinib inhibits the proliferation of MV4;11 and OC1-AML5 cells with IC50 of 8 nM and 14 nM, respectively, and induces apoptosis in a dose-dependent manner. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
3T3 NEGyXWpMcW6jc3WgRZN{[Xl? M{PBdWlvcGmkaYTpc44hd2ZiUFTHSk1qdmS3Y3XkJGJz\FViaX7jc5Jxd3KjdHnvckB4cXSqIFnDOVAhd2ZiMD6wNFch|ryP MnTYNVI3PDZyMUm=
3T3 Ml;VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH6xeGVKdmirYnn0bY9vKG:oIGDsZZRmdGW2LXTldol3\WRiZ4Lve5RpKG[jY4TvdkBqdmS3Y3XkJFNVOyClZXzsJJBzd2yrZnXyZZRqd25id3n0bEBKSzVyIH;mJFAvODFizszN NYS3XZEyOTJ4NE[wNVk>
3T3 NH;xR4ZHfW6ldHnvckBCe3OjeR?= NUHrUW9VUW6qaXLpeIlwdiCxZjDWZZNkfWyjcjDlcoRwfGinbHnhcEBoem:5dHig[oFkfG:{IILlZ4VxfG:{IIfpeIghUUN3MDDv[kAxNjB3IN88US=> NXrtcVhQOTJ4NE[wNVk>
3T3 M3nPfGtqdmG|ZTDBd5NigQ>? MkLENlAhdWmw NFPIcVNFVVOR NGPFXJdE\WyudXzhdkBqdmirYnn0bY9vKG:oIG\FS2YhcW6mdXPl[EBpfW2jbjDLSHIheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCyNkDPxE1? MlfhNVYyPjJyMEi=
NIH3T3 MUfLbY5ie2ViQYPzZZk> NYTrXVVDOjBibXnu NVnBbY9HTE2VTx?= MUjpcohq[mm2IHj1cYFvKEuGUjDrbY5ie2ViZYjwdoV{e2WmIIfpeIghUUN3MDDv[kAxNjBzODFOwG0> NFLIXIUyPjF4MkCwPC=>
A549 M2LsXWZ2dmO2aX;uJGF{e2G7 M1LPdWROW09? M{TIb2lvcGmkaYTpc44hd2ZiYz3N[ZQh\GWyZX7k[Y51KEiJRj3pcoR2[2WmIHj1cYFvKEF3NEmgZ4VtdCCvaXfyZZRqd25id3n0bEBKSzVyIH;mJFIh|ryP NVPS[45VOTh2M{SxOFU>
DU145 M4P5T2Z2dmO2aX;uJGF{e2G7 MYLEUXNQ NIPVZZVKdmirYnn0bY9vKG:oIHOtUYV1KGSncHXu[IVvfCCKR1[tbY5lfWOnZDDoeY1idiCGVUG0OUBk\WyuIIPjZZR1\XKrbnege4l1cCCLQ{WwJI9nKDFyIN88US=> MmPhNVg1OzRzNEW=
KB3-1 NUfs[YlIS3m2b4TvfIlkKEG|c3H5 NHLaRXE4OiCq M{LoR2ROW09? NY\sT41VS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWC2pcD3u[YdifGm4ZTDLRk0{NTFiY3XscJMhf2m2aDDJR|UxKG:oIEKuN{DPxE1? MoPvNVk{QTd|MkK=
KBV1 M1rZR2N6fG:2b4jpZ{BCe3OjeR?= MkHxO|IhcA>? NEDVPIVFVVOR MnfzR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVE1odHmlb4Dyc5RmcW5vZYjwdoV{e2mwZzDLRnYyKGOnbHzzJJdqfGhiSVO1NEBw\iB2LkGg{txO NIjMR|cyQTN7N{OyNi=>
A375 MVrDfZRwfG:6aXOgRZN{[Xl? M4jOdlczKGh? M4TXOmROW09? NY\KOWJCUUN3ME21MlQh|ryP NYj5NXpSOTl4NUS0NFg>
RS4-11 Ml33SpVv[3Srb36gRZN{[Xl? NHvhcVgzKGh? NVW0NYFlUW6qaXLpeIlwdiCxZjDGUHQ{KGG3dH;wbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvODB7OTFOwG0> NFnlRYwyQTZ3NESwPC=>
RS4-11 NGD2XmZHfW6ldHnvckBCe3OjeR?= MWmyJIg> MVLJcohq[mm2aX;uJI9nKE[OVEOgTXRFKG23dHHueEBifXSxcHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlA{PCEQvF2= Mn6zNVk3PTR2MEi=
Sf9 M1PlSWtqdmG|ZTDBd5NigQ>? NUmxV4R3OzBibXnu MXjJcohq[mm2aX;uJI9nKEeVVD30ZYdo\WRiVlXHSnIh\XiycnXzd4VlKHerdHigTWM2OCCxZjCwMlE5PSEQvF2= NEnRSpoyQTh3NEC1NS=>
Ba/F3 NVTBTIlGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVe0TJpSPzJiaB?= NIDS[4dKSzVyPUGuNkDPxE1? MnrjNlAyOTdyMES=
BaPTC2 M12zTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUH4WlNnPzJiaB?= M1zmfWlEPTB;MD6yNkDPxE1? M{L5cFIxOTF5MEC0
Sf9 Mn\hSpVv[3Srb36gRZN{[Xl? MWSxJIg> NGTBOIZFVVOR MmfiTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCKaYOteIFo\2WmIGLFWEBmgHC{ZYPz[YQhf2m2aDDJR|UxKG:oIEGuN{DPxE1? NYXKdHRsOjBzMUewNFQ>
H4 NXnZPIZtS3m2b4TvfIlkKEG|c3H5 MVSxNEDPxE1? M3;DOHRwgGmlaYT5JIlvKGi3bXHuJGg1KGOnbHzz MoDWNlA{PTB6ME[=
SF-539 M2TzN2tqdmG|ZTDBd5NigQ>? M1LZPFM{OyEQvF2= M2P6b|YxKG2rbh?= MoPySG1UVw>? NHP1fGdKdmirYnn0bY9vKG:oIGDES2ZT[mW2YTDwbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFEzNjJizszN NXLRfWdDOjB2MEO3NFA>
U251 NETSc4VMcW6jc3WgRZN{[Xl? NWXpT3d[OzN|IN88US=> Ml;2OlAhdWmw NGr6WlBFVVOR NIfsWlhKdmirYnn0bY9vKG:oIG\FS2ZTOiCyaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIEG4Mlkh|ryP MUeyNFQxOzdyMB?=
A431 NUHzWIRRU2mwYYPlJGF{e2G7 M2TiZ2lvcGmkaYTpc44hd2ZiUFTHSnJj\XSjIHX4dJJme3OnZDD3bZRpKEmFNUCgc4YhOTJwMjFOwG0> M{LiZlIxPTV6MEey
A431 Ml\ET4lv[XOnIFHzd4F6 M2HvW2lvcGmkaYTpc44hd2ZiVlXHSnIzKGW6cILld5Nm\CC5aYToJGlEPTBib3[gNVgvQSEQvF2= NHLKXoUzODV3OEC3Ni=>
HepG2 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1iwbVczKGh? M1nDUWlEPTB;Mz64NUDPxE1? MlPJNlA2PzB3Mk[=
Kasumi-1 NHnyTYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnu5O|IhcA>? NE\FWmtKSzVyPUCuNFE3KM7:TR?= M3zKWlIxPTdyNUK2
RS4-11 NEi2NIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHMO|IhcA>? MojpTWM2OD1zIN88US=> MVqyNFU4ODV{Nh?=
THP1 NV[zNpFXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXP6eooxPzJiaB?= M4PyU2lEPTB;MD61JO69VQ>? MnPRNlA2PzB3Mk[=
Kasumi-1 NVnZWZhLTnWwY4Tpc44hSXO|YYm= NWfQVWJ6UW6qaXLpeIlwdiCxZjDjMWtqfCCjdYTvdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjBzNTFOwG0> MXmyNFg{OzB|OR?=
A549 MmDHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTFXXA4OTZiaB?= MmjoRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\Wyucx?= M4jOUlIyPDVyNE[z
HL60 NVrCXJU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nvUlE3KGh? MY\BcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTE[wJINmdGy| NU\KOZhrOjF2NUC0OlM>
HUVEC NVTOdpNtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUGxOkBp NUTRd4J6UW6qaXLpeIlwdiCxZjDWSWdHNWmwZIXj[YQh[2WubDDwdo9tcW[ncnH0bY9vKHerdHigTWM2OCCxZjCyMlc2KM7:TR?= Moj2NlE1PTB2NkO=
HUVEC MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHobIkyPiCq MoP4TY5pcWKrdHnvckBw\iCkRlfGMYlv\HWlZXSgZ4VtdCCycn;sbYZmemG2aX;uJJdqfGhiSVO1NEBw\iB2LkC0JO69VQ>? NVKzd2F7OjF2NUC0OlM>
IM9 NXzIT2F3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWixOkBp M176WWFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFnNPUBk\Wyucx?= MWmyNVQ2ODR4Mx?=
K562 M3jpNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIGyc44yPiCq NYLtWFV1SW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gT|U3OiClZXzsdy=> NHTYSnkzOTR3MES2Ny=>
MDA-MB-231 M1jZXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY[yVm91OTZiaB?= NFHmSmtCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy| MUKyNVQ2ODR4Mx?=
H460 NHHqTVREgXSxdH;4bYMhSXO|YYm= NWTHPHp2PzJiaB?= NET2em1KSzVyPUKuO{DPxE1? NFfrSpczOTZ{MUi4NC=>
SMMC7721 NGG5cYdEgXSxdH;4bYMhSXO|YYm= NHywR4Q4OiCq NV;3THNmUUN3ME22MlQ4KM7:TR?= NIjF[VQzOTZ{MUi4NC=>
WI38 NYHoRnRtS3m2b4TvfIlkKEG|c3H5 M2HT[VczKGh? NEW3PWVKSzVyPUiuOVYh|ryP MmrmNlE3OjF6OEC=
HEK293 MnzpT4lv[XOnIFHzd4F6 MoP2NVAxKG6P MlnqNUBp NGO5SW1ld2W|IH7veEBqdmirYnn0JHZGT0ZvaX7keYNm\CCjdYTvdIhwe3Cqb4L5cIF1cW:wIH;mJJR6em:|aX7lJFEyPzVicnXzbYR2\SCxbjDWSWdHWjJiZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[Yxtew>? M3jqTlIyQDh3Mki3
HUVEC NHrkT5ZHfW6ldHnvckBCe3OjeR?= MW[xJO69VQ>? MonMNlQhcA>? NVGxdIVtSW62aXHu[4lw\2WwaXOgZYN1cX[rdImgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iVlXHSk1qdmS3Y3XkJINmdGxibXnndoF1cW:w NVv4c4NNOjF7NkOzNFU>
HUVEC MmXkSpVv[3Srb36gRZN{[Xl? NI[5bIIyKM7:TR?= MkfmNUBp M{XRT2lvcGmkaYTpc44hd2ZiRWLLJJBpd3OyaH;yfYxifGmxbjDheEBVcHJ{MEKvWJlzOjB2IHnuJHZGT0Zvc4TpcZVt[XSnZDDIWXZGSw>? MmfHNlE6PjN|MEW=
HUVEC MmXmSpVv[3Srb36gRZN{[Xl? MXmxJO69VQ>? Mnz3NUBp MmnpTY5pcWKrdHnvckBw\iCnTl;TJJBpd3OyaH;yfYxifGmxbjDheEBU\XJvMUG3NkBqdiCYRVfGMZN1cW23bHH0[YQhUFWYRVO= NUHRSoR3OjF7NkOzNFU>
HUVEC MV7LbY5ie2ViQYPzZZk> NUmwe2VwOSEQvF2= M{jXUVEhcA>? NHLyTmxKdmirYnn0bY9vKG:oIG\FS2ZTOiCyaH;zdIhwenmuYYTpc44h[XRidInyMVEyPzViaX6gWmVITi2|dHnteYxifGWmIFjVWmVE M3fER|IyQTZ|M{C1
HUVEC MYXGeY5kfGmxbjDBd5NigQ>? MlHoNUDPxE1? M17GN|EhcA>? MVXkc4V{KG6xdDDpcohq[mm2IFHLWEBxcG:|cHjvdplt[XSrb36gZZQhW2W{LUS3N{BqdiCYRVfGMZN1cW23bHH0[YQhUFWYRVO= M1PnVlIyQTZ|M{C1
HL60 MmHGR5l1d3SxeHnjJGF{e2G7 MmjyOVAh|ryP NUHk[IVuPDhiaB?= NWXsVGpQTE2VTx?= NF:zPFBKSzVyPUG1MlUh|ryP NULEVoFjOjJyMUmxPFg>
K562 Mon3R5l1d3SxeHnjJGF{e2G7 NHjuPGw2OCEQvF2= NFjyWVI1QCCq NWftc25RTE2VTx?= M1zhb2lEPTB;MkGuPUDPxE1? NF[1UYozOjBzOUG4PC=>
PC3 MnnBR5l1d3SxeHnjJGF{e2G7 NGrMVWM2OCEQvF2= MWG0PEBp NF[zfHNFVVOR NIXqSIRKSzVyPUK1MlEh|ryP MX6yNlAyQTF6OB?=
SF-539 Mlj6T4lv[XOnIFHzd4F6 NF73ZoM{OzNizszN Ml;hOlAhdWmw M4HRSWlvcGmkaYTpc44hd2ZiUFTHSnJj\XSjIIT5do9{cW6nIHvpcoF{\SCjY4Tpeol1gSCrbjDQSGdHNUKELYP0bY12dGG2ZXSgbJVu[W5iU1[tOVM6KGOnbHzzJJdqfGhiSVO1NEBw\iBzMj6yJO69VQ>? NYTmWo83OjJ{MES3OFE>
HAEC M2TBXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDZNVAxKM7:TR?= Mnj3O|IhcA>? MnPGRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQVXDJINmdGy|IHX4dJJme3OrbnegWmVITlJid3n0bEBKSzVyIH;mJFAvOSEQvF2= NULZ[GxTOjJ2NES2O|k>
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MV4-11 NXnOb2hXS3m2b4TvfIlkKEG|c3H5 MkLkO|IhcA>? MUfJR|UxRTBwMECzJO69VQ>? NGTKR5EzOjR3MkWxPC=>
HepG2 NYDqO21NS3m2b4TvfIlkKEG|c3H5 Moi2OFghcA>? M3T5TGlEPTB;MUOuNlQh|ryP NGLRbHczOjR6M{[wPC=>
PC9 NWHsSY1qS3m2b4TvfIlkKEG|c3H5 MUS0PEBp NWjIdpRnUUN3ME2xNE46PyEQvF2= NILyU3kzOjR6M{[wPC=>
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MCF7 NIjISnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXYO4gyODBizszN MkT5OFghcA>? NVv5fVBjTE2VTx?= MXTHTVUyRTJizszN MUCyNlU3ODZ{Nx?=
MDA-MB-435 M3Lme2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTBNVAxKM7:TR?= MlXROFghcA>? NGrPXlBFVVOR NITZe4hIUTV{PUKg{txO NFrQSmkzOjV4ME[yOy=>
OVCAR3 M13MS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPlUGs1OTByIN88US=> NHPRXpM1QCCq M{O2[WROW09? Mle4S2k2Oz1|LkKg{txO MnzINlI2PjB4Mke=
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SW620 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PtTVExOCEQvF2= MoS5OFghcA>? M2TpT2ROW09? NULDPGtIT0l3NU2xMlMh|ryP MWWyNlU3ODZ{Nx?=
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UACC257 NWn2RZNTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX:zbnRWOTByIN88US=> Mn3OOFghcA>? NHv3XlhFVVOR M{fPcmdKPTd;NDFOwG0> NH7JUlIzOjV4ME[yOy=>
HAEC NWLDVlRQS3m2b4TvfIlkKEG|c3H5 NUPE[4VCOTByIN88US=> MX:3NkBp MmW2SG1UVw>? NXzUPJZGS3m2b4TvfIlkcXS7IHHnZYlve3RiVlXHSnIh\XiycnXzd4lv\yCKQVXDJJdqfGhiSVO1NEBw\iByLkGg{txO M4XESVI{OTNzNUSx
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HUVEC NXfNfHN4TnWwY4Tpc44hSXO|YYm= MmXyNkDPxE1? NH3uS20yQCCq NHvYcXBFVVOR MY\BcpRq[W6paX;n[Y5q[yCjY4Tpeol1gSCrbjDIWXZGS3NidX7k[ZIhcHmyb4jpZ{Bkd26maYTpc44h[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB1fWKnIH\vdo1ifGmxbh?= NEnmNHYzOzF3M{KwNC=>
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A498 NYnSXoc4S3m2b4TvfIlkKEG|c3H5 M37WZVExOCEQvF2= M1SyR|czKGh? NI\FUI5FVVOR MXLJR|UxRTRwMzFOwG0> MVmyN|Q5QTZ{Nh?=
HUVEC MkHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVWzJO69VQ>? MnW3NlQhcA>? M4PrSGROW09? NWjWdpg2SW62aXHu[4lw\2WwaXOgZYN1cX[rdImgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDWSWdHNWmwZIXj[YQhfHWkZTDmc5Ju[XSrb36ge4l1cCCHQ{WwJI9nKDBwNkS1JO69VQ>? MnHrNlM2QDN7MUG=
HUVEC NU\5XohFU2mwYYPlJGF{e2G7 MkT3NlAxKM7:TR?= M4HCNGROW09? NXW1cFc2UW6qaXLpeIlwdiCxZjDWSWdHWjJicHjvd5Bpd3K7bHH0bY9vKGmwIHfyc5d1cCCoYXP0c5Iue3SrbYXsZZRm\CCKVW\FRy=> M37V[FI{PTh|OUGx
HUVEC MoTiT4lv[XOnIFHzd4F6 NFrGfYEzODBizszN MWLEUXNQ NIXhem5KdmirYnn0bY9vKG:oIG\FS2ZTOSCyaH;zdIhwenmuYYTpc44hcW5iZ4Lve5RpKG[jY4Tvdk1{fGmvdXzheIVlKEiXVlXD NFvhV2gzOzV6M{mxNS=>
A549 MU\DfZRwfG:6aXOgRZN{[Xl? MVG3NkBp M3PmXGROW09? NXLUXXByUUN3ME2yMlQ1KM7:TR?= MXuyN|YxOjR2MR?=
HCT116 NUjrTIIyS3m2b4TvfIlkKEG|c3H5 NETEbmQ4OiCq MkDOSG1UVw>? NG[0XJpKSzVyPUSuO|Eh|ryP M1XZRVI{PjB{NESx
MCF7 NU\LO2x[S3m2b4TvfIlkKEG|c3H5 M3Xvd|czKGh? M2jTSGROW09? MnLDTWM2OD14LkK5JO69VQ>? NFfUVWgzOzZyMkS0NS=>
BGC NGDVS|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7qUoI1PzJiaB?= MV;EUXNQ NUnYV41wUUN3ME20Mlc5KM7:TR?= NG[wc4YzOzl7OUC0NC=>
BxPC3 MlzrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrlO|IhcA>? M{jPZWROW09? M3y1cWlEPTB;Mz62N{DPxE1? MmTnNlM6QTlyNEC=
HT-29 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLPZo9GPzJiaB?= NWXpZ3N3TE2VTx?= M2nZOmlEPTB;MT60O{DPxE1? NFXtfIszOzl7OUC0NC=>
T24 M37rU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUm3NkBp MlL3SG1UVw>? MmHxTWM2OD1{LkS0JO69VQ>? MmPTNlM6QTlyNEC=
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MCF7 MoTjR5l1d3SxeHnjJGF{e2G7 NHe0[mE4OiCq MYXEUXNQ NU\uSZhVUUN3ME2wMlAzPzFizszN NXL2ZVhOOjR6OUC2OVI>
MCF7 MlzmR5l1d3SxeHnjJGF{e2G7 NIjt[VY4OiCq NG\BUWhFVVOR NUi1S5VbUUN3ME2wMlAzQTNizszN NHfCZ|gzPDh7ME[1Ni=>
MDA-MB-231 NFX3PY9EgXSxdH;4bYMhSXO|YYm= NFy1d5I4OiCq NI\VTZZFVVOR M3LjOWlEPTB;MD6wNlI{KM7:TR?= MYKyOFg6ODZ3Mh?=
MDA-MB-435 MYjDfZRwfG:6aXOgRZN{[Xl? NFj1Znk4OiCq NUnnc3E4TE2VTx?= NXvXW|JJUUN3ME2wMlAxQTdizszN MoTNNlQ5QTB4NUK=
MDA-MB-468 M2DXd2N6fG:2b4jpZ{BCe3OjeR?= M{jzNlczKGh? M{LXbWROW09? MYjJR|UxRTBwMEC2NUDPxE1? M1jCblI1QDlyNkWy
A431 NE\RU|RMcW6jc3WgRZN{[Xl? NV;qb5RSOTBizszN MYWxJIg> NGrRUJFFVVOR MXfJcohq[mm2aX;uJI9nKEWJRmKge4l1cCCLQ{WwJI9nKDBwMUeyNUDPxE1? MmD2NlQ5QTB4NUK=
SH-SY5Y NYTPdJg{U2mwYYPlJGF{e2G7 NWXmblZ6OTBizszN MorsNUBp MXnEUXNQ M2L6dWlvcGmkaYTpc44hd2ZiUFTHSnJj\XSjIIfpeIghUUN3MDDv[kAxNjB6M{Gg{txO M2PENlI1QDlyNkWy
U251 NHHkUFZMcW6jc3WgRZN{[Xl? NX;MS4ZJOTBizszN Ml30NUBp NV3vVFJSTE2VTx?= NIOzWmZKdmirYnn0bY9vKG:oIG\FS2ZTOiC5aYToJGlEPTBib3[gNE4xOTh7IN88US=> M{fvVlI1QDlyNkWy
Bel7402 Mnr0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DKOFczKGh? NHTON2lFVVOR MVrJR|UxRTJwNkeg{txO NI\RR2UzPDlyNEm2NS=>
HK2 NILLU3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIG4[2k4OiCq MYjEUXNQ MnLsTWM2OD13Lki1JO69VQ>? MVuyOFkxPDl4MR?=
LO2 MlzNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrCTHpwPzJiaB?= M3W0VGROW09? M4jzTWlEPTB;MUmuPVMh|ryP M1r1fVI1QTB2OU[x
MV4-11 NGTMTmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zBdlQ5KGh? MonZSG1UVw>? NInvdWNKSzVyPUCuNFA{KM7:TR?= M3O5WVI1QTB2OU[x
NCI-H3122 Mn;qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rBXVczKGh? NGTOW3ZFVVOR NGT3RVZKSzVyPUCuPFMh|ryP NUDNSnlvOjR7MES5OlE>
NCI-H460 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\xOWw4OiCq M3:5XWROW09? NUHReYNlUUN3ME20MlMyKM7:TR?= NVfqNWJ5OjR7MES5OlE>
NCI-H526 M1[xTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HiXVczKGh? NXjrW|VWTE2VTx?= NGX2W25KSzVyPUGuNFEh|ryP MmXNNlQ6ODR7NkG=
TT MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\MNZBpPzJiaB?= NW\3cJJoTE2VTx?= NHPydoFKSzVyPUCuNFQh|ryP MUGyOFkxPDl4MR?=
EoL-1-cell MmLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDDUnhOUUN3ME2xMlY1KHCP M4XLcHNCVkeHUh?=
MV-4-11 M17CeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rqSWlEPTB;MkeyJJBO MU\TRW5ITVJ?
NOS-1 MljYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrWTWM2OD1zNT6zJI5O MYXTRW5ITVJ?
CGTH-W-1 M2XKcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITG[2tKSzVyPUOwMlk1KG6P NYTPToJpW0GQR1XS
MONO-MAC-6 NUTjNYhTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPiXFJKSzVyPUOzMlghdk1? NWDVfo5sW0GQR1XS
ALL-PO MkTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moi5TWM2OD15OT64PUBvVQ>? M17ET3NCVkeHUh?=
NKM-1 M4fuRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTl6LkWyJI5O MXTTRW5ITVJ?
KM12 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NISw[3hKSzVyPUO1NE4yPCCwTR?= M1rDW3NCVkeHUh?=
TE-15 NXfM[WFHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzsTWM2OD13MEeuOlEhdk1? MXHTRW5ITVJ?
697 MnLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTZzND6yOUBvVQ>? NYfUV3dzW0GQR1XS
MOLT-16 MnHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoW2TWM2OD14M{GuN|Ihdk1? Mo[5V2FPT0WU
GB-1 NHPOXlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTdzMD6yN{BvVQ>? NFPR[XRUSU6JRWK=
TE-12 M{ixdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIO2emhKSzVyPUiwOE42PSCwTR?= M3PnWnNCVkeHUh?=
ES6 NUWzSlFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofMTWM2OD17OEGuNFYhdk1? NGHEN2FUSU6JRWK=
LC-2-ad MoW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrvTWM2OD1zLkGxOFA4KM7:TR?= M2PycHNCVkeHUh?=
BL-70 NUfFUW9ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHSxVHRKSzVyPUGuNVE5PDZizszN MVXTRW5ITVJ?
ETK-1 NHTmOmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDwb25KSzVyPUGuNlg2QCEQvF2= NXTFNoM{W0GQR1XS
A4-Fuk MmP4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVL0b|BiUUN3ME2xMlM1OTRzIN88US=> MnrXV2FPT0WU
OCI-AML2 NIrn[4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfFdGhkUUN3ME2xMlM3QDVzIN88US=> M37URXNCVkeHUh?=
SIG-M5 NELkN5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH:wSW5KSzVyPUGuN|cxODlizszN MUPTRW5ITVJ?
NCI-SNU-16 Mke1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfyVWdXUUN3ME2xMlQ3PDh4IN88US=> NFLtU25USU6JRWK=
PSN1 NXvEXXZ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTFwNUC2O|Yh|ryP MV\TRW5ITVJ?
SR Ml3LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIGwR2hKSzVyPUGuOVQ2PzJizszN MnLIV2FPT0WU
A3-KAW NH;LcphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HJdWlEPTB;MT62NlU1PiEQvF2= NHzKeG9USU6JRWK=
KS-1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rtSmlEPTB;MT62PVI1PyEQvF2= NG\XSZJUSU6JRWK=
CTV-1 M4TpS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTFwN{K3OVEh|ryP NVnUO|E5W0GQR1XS
LB1047-RCC NV35bFE4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTFwOEG2NlQh|ryP M4PKZ3NCVkeHUh?=
EMG-01 NH;BN4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGGyOHNKSzVyPUGuPFM2PjNizszN NX3uO2ljW0GQR1XS
TE-11 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nsbGlEPTB;MT64N|k5PSEQvF2= M3P4WHNCVkeHUh?=
CMK MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETYZm9KSzVyPUGuPVU2OTdizszN NFj1V4VUSU6JRWK=
NB1 M1\DOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjrbndEUUN3ME2xMlk3OTF5IN88US=> M17Jc3NCVkeHUh?=
HAL-01 M3Tw[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nZNGlEPTB;Mj6wOVk1PiEQvF2= NFP2TodUSU6JRWK=
DEL NE\tPHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jIXmlEPTB;Mj6wPFQ5OiEQvF2= NGfHOGVUSU6JRWK=
RL95-2 MmG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvmdpQ6UUN3ME2yMlEyOTN5IN88US=> NHPsfYlUSU6JRWK=
KARPAS-299 NFLkW3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPZfGFGUUN3ME2yMlEyOzF|IN88US=> MkPRV2FPT0WU
EW-16 NWi0d4NVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjLeldKSzVyPUKuNVM2ODhizszN M2\5cnNCVkeHUh?=
RS4-11 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkX5TWM2OD1{LkG3PVI1KM7:TR?= MmDNV2FPT0WU
BB30-HNC MlruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnzTWM2OD1{LkKyN|c2KM7:TR?= NV3vRplIW0GQR1XS
DOHH-2 NYHlPWVOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTJwM{O0N|Eh|ryP NEXDfJhUSU6JRWK=
RPMI-8402 MlnLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTVTWM2OD1{LkOzOlE5KM7:TR?= NEjVO2RUSU6JRWK=
BV-173 M2S1TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTEW2lMUUN3ME2yMlM{PjZizszN NVnxc4ZwW0GQR1XS
TE-10 MmfVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIr1bodKSzVyPUKuN|Q{QDRizszN NH;ReYhUSU6JRWK=
TE-8 M4DNc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTJwM{ewN|gh|ryP M2DqfHNCVkeHUh?=
K052 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHO2eHNKSzVyPUKuOFAzODJizszN NVPNWWo{W0GQR1XS
KARPAS-45 NYf1eIx1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUn6XpFQUUN3ME2yMlQ6PDR4IN88US=> NYroeVlwW0GQR1XS
SK-NEP-1 NUDDOW9bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLUNnhYUUN3ME2yMlYxOjN5IN88US=> NVS3S|RlW0GQR1XS
KGN MnHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTJwNkCzN|kh|ryP NGLhd2ZUSU6JRWK=
ML-2 MlSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrNTWM2OD1{Lk[zOVEzKM7:TR?= M4PofnNCVkeHUh?=
LAMA-84 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH30S3hKSzVyPUKuOlk2PDVizszN MkG0V2FPT0WU
LXF-289 NETYXodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTJwN{K5PFkh|ryP MnPCV2FPT0WU
A101D M4f0T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkK3TWM2OD1{Lke4N|A1KM7:TR?= NUTvbm9IW0GQR1XS
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SK-N-FI NGPuXXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzVTWM2OD1zNz62PVE{KM7:TR?= NV[4eo5RW0GQR1XS
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NCI-H1882 NV7sNGlZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHMeYc1UUN3ME2xO{46QDN2IN88US=> M1f1fXNCVkeHUh?=
A704 NH\GNmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LJWGlEPTB;MUeuPVkxPCEQvF2= Mn3VV2FPT0WU
L-428 M{DOUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPle2dKSzVyPUG4MlAyPTFizszN NXHPU2puW0GQR1XS
HCC1187 M{jSXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fLXWlEPTB;MUiuNFE5PyEQvF2= MYfTRW5ITVJ?
NCI-H1581 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnqTWM2OD1zOD6wPFY3KM7:TR?= MYjTRW5ITVJ?
BB65-RCC NGjCPW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWW1XINnUUN3ME2xPE41OTZ{IN88US=> MoLLV2FPT0WU
EM-2 M1mwcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTF6LkW2O|Ih|ryP MV;TRW5ITVJ?
Raji MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTF7Lkm1OlUh|ryP NXWzbIVuW0GQR1XS
TE-1 MorUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojVTWM2OD1{MD60NVA1KM7:TR?= M3Xtc3NCVkeHUh?=
SW962 M{n0SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrKTWM2OD1{MD60Nlk{KM7:TR?= MUTTRW5ITVJ?
MHH-NB-11 Ml3CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zNb2lEPTB;MkCuOVUzOSEQvF2= MWrTRW5ITVJ?
no-10 M{j0bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XOPWlEPTB;MkGuNFI3PCEQvF2= NXy1[HliW0GQR1XS
GDM-1 NUTZXHdGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfhUnlLUUN3ME2yNU46PDF2IN88US=> MUTTRW5ITVJ?
KMS-12-PE NHvuNnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mle5TWM2OD1{Mj6yO|Qh|ryP NH:3XJhUSU6JRWK=
NCI-H510A MlHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnXTWM2OD1{ND6xNlc5KM7:TR?= MXzTRW5ITVJ?
ES5 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETufGZKSzVyPUK0Mlc{PDlizszN NXTjPWVZW0GQR1XS
JiyoyeP-2003 NX33eGV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3VTWM2OD1{Nj6yO|QzKM7:TR?= NXXSXWR1W0GQR1XS
NMC-G1 NGD2PVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3BSnpKSzVyPUK3MlE5OjJizszN M2D3VHNCVkeHUh?=
NCI-H446 NUj2[2F1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorhTWM2OD1{Nz60PVQ3KM7:TR?= NYizZolwW0GQR1XS
NB7 M{HoW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTJ5LkmyNlkh|ryP MWPTRW5ITVJ?
A388 MnryS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTJ6LkCwO|Qh|ryP MYXTRW5ITVJ?
JVM-2 MmrLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVX0PWNJUUN3ME2yPE4zQDl6IN88US=> M4L6SnNCVkeHUh?=
HT-144 M4S5XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfp[FE6UUN3ME2yPE43QSEQvF2= M4juXXNCVkeHUh?=
NCI-H747 M1PLWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXaSpBKUUN3ME2yPE46OTl3IN88US=> MXTTRW5ITVJ?
NCI-H1650 MkPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\jbGlEPTB;MkmuNFE4PiEQvF2= NGC1UFBUSU6JRWK=
EB-3 MkLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH23WWNKSzVyPUK5MlU{ODlizszN MYHTRW5ITVJ?
KLE NXTkRXVGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvmdFlKSzVyPUK5MlYyQSEQvF2= NYfaN3NoW0GQR1XS
TK10 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTITWM2OD1|MD6xNlYh|ryP NVLOdmtkW0GQR1XS
COLO-668 NVTmNWV{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnnPWJKSzVyPUOwMlc6OiEQvF2= MU\TRW5ITVJ?
NCI-H23 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTNzLkGwOlMh|ryP NHfiWHhUSU6JRWK=
GOTO NHvlN3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTNzLk[wPFUh|ryP MYrTRW5ITVJ?
MSTO-211H NYPXbFVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXpU|R7UUN3ME2zNU45Pjd6IN88US=> NHO2TolUSU6JRWK=
LB831-BLC Mn;JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLLUHpKSzVyPUOyMlM5PDNizszN MWnTRW5ITVJ?
SCH NV3l[3BFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXqTWM2OD1|Mj64OFg2KM7:TR?= NILzUlBUSU6JRWK=
EHEB MnHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHvZoVKSzVyPUO0MlEyQTNizszN NXTkfG1HW0GQR1XS
U-266 NEjidW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHTPYFQUUN3ME2zOE4zPzhzIN88US=> MWHTRW5ITVJ?
EW-11 MmPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEexfXlKSzVyPUO0MlQ4OjVizszN MXfTRW5ITVJ?
TE-9 Mo\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;KTWM2OD1|Nz6wOFAyKM7:TR?= NGGwTFJUSU6JRWK=
ES3 NUHwdYU5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfX[Jh6UUN3ME2zO{42ODB2IN88US=> MoS5V2FPT0WU
NCI-H2141 M{X4O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHtXW9{UUN3ME2zPE4xQDR|IN88US=> NX[0O3JwW0GQR1XS
MPP-89 NWPTOpdXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XDcWlEPTB;NEKuNFU5PiEQvF2= M4OweXNCVkeHUh?=
SK-MEL-2 NYTrdVNXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PYUGlEPTB;NEKuOlQxPSEQvF2= NUnSUYNsW0GQR1XS
LC-1F M3\rWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHJTWM2OD12Mz6zOlgzKM7:TR?= NV:zbZEzW0GQR1XS
NH-12 NIPye2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{GweWlEPTB;NEOuPVM2QSEQvF2= NInrWI9USU6JRWK=
RKO MkXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWr4bm03UUN3ME20OE4yOjV{IN88US=> NXrsXYxCW0GQR1XS
KM-H2 NGLPSJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TpV2lEPTB;NESuPVU4PyEQvF2= M3n1U3NCVkeHUh?=
SK-UT-1 M3TtTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjKe|RKSzVyPUS5Mlg5OjVizszN MmfiV2FPT0WU

... Click to View More Cell Line Experimental Data

In vivo Consistent with the substantial and selective inhibition of VEGFR2 or PDGFR phosphorylation and signaling in vivo, Sunitinib (20-80 mg/kg/day) exhibits broad and potent dose-dependent anti-tumor activity against a variety of tumor xenograft models including HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435. Sunitinib dosing at 80 mg/kg/day for 21 days leads to complete tumor regression in six of eight mice, without tumor re-growing during a 110-day observation period after the end of treatment. Second round of treatment with Sunitinib remains efficacious against tumors that are not fully regressed during the first round of treatment. Sunitinib treatment results in significant decrease in tumor MVD, with ~40% reduction in SF763T glioma tumors. SU11248 treatment results in a complete inhibition of additional tumor growth of luciferase-expressing PC-3M xenografts, despite no reduction in tumor size. [2] Sunitinib treatment (20 mg/kg/day) dramatically suppresses the growth subcutaneous MV4;11 (FLT3-ITD) xenografts and prolongs survival in the FLT3-ITD bone marrow engraftment model. [3]

Protocol

Kinase Assay:[1]
+ Expand

Biochemical Tyrosine Kinase Assays:

IC50 values for Sunitinib against VEGFR2 (Flk-1) and PDGFRβ are determined using glutathione S-transferasefusion proteins containing the complete cytoplasmic domain of the RTK. Biochemical tyrosine kinase assays to quantitate the trans-phosphorylation activity of VEGFR2 (Flk-1) and PDGFRβ are performed in 96-well microtiter plates precoated (20 μg/well in PBS; incubated overnight at 4 °C) with the peptide substrate poly-Glu,Tyr (4:1). Excess protein binding sites are blocked with the addition of 1-5% (w/v) BSA in PBS. Purified GST-fusion proteins are produced in baculovirus-infected insect cells. GST-VEGFR2 and GST-PDGFRβ are then added to the microtiter wells in 2 × concentration kinase dilution buffer consisting of 100 mM HEPES, 50 mM NaCl, 40 μM NaVO4, and 0.02% (w/v) BSA. The final enzyme concentration for GST-VEGFR2 or GST-PDGFRβ is 50 ng/mL. Twenty-five μL of diluted Sunitinib are subsequently added to each reaction well to produce a range of inhibitor concentrations appropriate for each enzyme. The kinase reaction is initiated by the addition of different concentrations of ATP in a solution of MnCl2 so that the final ATP concentrations spanned the Km for the enzyme, and the final concentration of MnCl2 is 10 mM. The plates are incubated for 5-15 minutes at room temperature before stopping the reaction with the addition of EDTA. The plates are then washed three times with TBST. Rabbit polyclonal antiphosphotyrosine antisera are added to the wells at a 1:10,000 dilution in TBST containing 0.5% (w/v) BSA, 0.025% (w/v) nonfat dry milk, and 100 μM NaVO4 and incubated for 1 hour at 37 °C. The plates are then washed three times with TBST, followed by the addition of goat antirabbit antisera conjugated with horseradish peroxidase (1:10,000 dilution in TBST). The plates are incubated for 1 hour at 37 °C and then washed three times with TBST. The amount of phosphotyrosine in each well is quantitated after the addition of 2,2′-azino-di-[3-ethylbenzthiazoline sulfonate] as substrate.
Cell Research:[3]
+ Expand
  • Cell lines: RS4;11, MV4;11, and OC1-AML5
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 24 and 48 hours
  • Method: Cells are starved overnight in medium containing 0.1% FBS prior to addition of Sunitinib and FL (50 ng/mL; FLT3-WT cells only). Proliferation is measured after 48 hours of culture using the Alamar Blue assay or trypan blue cell viability assays. Apoptosis is measured 24 hours after Sunitinib addition by Western blotting to detect cleavage of poly (ADP-ribose) polymerase (PARP) or levels of caspase-3.
    (Only for Reference)
Animal Research:[2]
+ Expand
  • Animal Models: Female nu/nu mice implanted s.c. with HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435, and male nu/nu mice bearing luciferase-expressing PC-3M tumors
  • Formulation: Formulated as a carboxymethyl cellulose suspension or as a citrate buffered (pH 3.5) solution
  • Dosages: ~80 mg/kg
  • Administration: Orally once daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 15 mg/mL (28.16 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
2mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 532.56
Formula

C22H27FN4O2.C4H6O5

CAS No. 341031-54-7
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02761057 Recruiting Recurrent Renal Cell Carcinoma|Stage III Renal Cell Cancer|Stage IV Renal Cell Cancer|Type 1 Papillary Renal Cell Carcinoma|Type 2 Papillary Renal Cell Carcinoma National Cancer Institute (NCI) April 2016 Phase 2
NCT02779283 Recruiting Untreated Adult Acute Myeloid Leukemia OHSU Knight Cancer Institute|National Cancer Institute (NCI) December 2015 Phase 1
NCT02626754 Enrolling by invitation Renal Cell Carcinoma vghtpe user|Taipei Veterans General Hospital, Taiwan August 2015 Phase 2
NCT02465060 Recruiting Advanced Malignant Neoplasm|Lymphoma|Recurrent Plasma Cell Myeloma|Recurrent Solid Neoplasm|Refractory Malignant Neoplasm|Refractory Plasma Cell Myeloma National Cancer Institute (NCI) August 2015 Phase 2
NCT01835158 Active, not recruiting Clear Cell Renal Cell Carcinoma|Metastatic Renal Cell Cancer|Stage III Renal Cell Cancer|Stage IV Renal Cell Cancer National Cancer Institute (NCI) July 2013 Phase 2
NCT01740154 Terminated Fatigue|Recurrent Renal Cell Cancer|Stage IV Renal Cell Cancer Case Comprehensive Cancer Center|National Cancer Institute (NCI) September 2012 --

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    I was wondering that the compound is in its cis or trans form?

  • Answer:

    S1042 Sunitinib Malate is Z form.

  • Question 2:

    What is the difference between Sunitinib Malate(S1042) and Sunitinib(S7781)?

  • Answer:

    S1042 is the Malate salt form of Sunitinib. The biological activities of these two compounds are the same but the solubility of these two compounds in aqueous solvent are different.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID